Mutant Browser

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Protein name Generic number Position Segment Mutation FoldChange or Qual Exp Type Ligand Reference Review
5ht4r_human 4.53x53 149 TM4 P => A Abolished K(d) (Binding - Radioligand saturation) GR 113808 Mialet J et al (2000)
5ht4r_human 5.43x44 197 TM5 S => A Abolished K(d) (Binding - Radioligand saturation) GR 113808 Mialet J et al (2000)
5ht4r_human 6.51x51 275 TM6 F => A Abolished K(d) (Binding - Radioligand saturation) GR 113808 Mialet J et al (2000)
5ht4r_human 7.43x42 302 TM7 Y => A Abolished K(d) (Binding - Radioligand saturation) GR 113808 Mialet J et al (2000)
5ht4r_human 2.50x50 66 TM2 D => N Unchanged Single-point (Functional - cAMP accumulation) 5-hydroxytryptamine Mialet J et al (2000)
5ht4r_human 3.32x32 100 TM3 D => N Abolished Single-point (Functional - cAMP accumulation) 5-hydroxytryptamine Mialet J et al (2000)
5ht4r_human 4.53x53 149 TM4 P => A Unchanged Single-point (Functional - cAMP accumulation) 5-hydroxytryptamine Mialet J et al (2000)
5ht4r_human 4.54x54 150 TM4 T => V Unchanged Single-point (Functional - cAMP accumulation) 5-hydroxytryptamine Mialet J et al (2000)
5ht4r_human 4.57x57 153 TM4 S => A Unchanged Single-point (Functional - cAMP accumulation) 5-hydroxytryptamine Mialet J et al (2000)
5ht4r_human 5.42x43 196 TM5 C => A Unchanged Single-point (Functional - cAMP accumulation) 5-hydroxytryptamine Mialet J et al (2000)
5ht4r_human 5.43x44 197 TM5 S => A Abolished Single-point (Functional - cAMP accumulation) 5-hydroxytryptamine Mialet J et al (2000)
5ht4r_human 6.51x51 275 TM6 F => A Unchanged Single-point (Functional - cAMP accumulation) 5-hydroxytryptamine Mialet J et al (2000)
5ht4r_human 6.52x52 276 TM6 F => V Unchanged Single-point (Functional - cAMP accumulation) 5-hydroxytryptamine Mialet J et al (2000)
5ht4r_human 6.55x55 279 TM6 N => L Unchanged Single-point (Functional - cAMP accumulation) 5-hydroxytryptamine Mialet J et al (2000)
5ht4r_human 7.43x42 302 TM7 Y => A Abolished Single-point (Functional - cAMP accumulation) 5-hydroxytryptamine Mialet J et al (2000)
5ht4r_human 2.50x50 66 TM2 D => N N/A N/A Mialet J et al (2000)
5ht4r_human 3.32x32 100 TM3 D => N N/A N/A Mialet J et al (2000)
5ht4r_human 4.53x53 149 TM4 P => A N/A N/A Mialet J et al (2000)
5ht4r_human 4.54x54 150 TM4 T => V N/A N/A Mialet J et al (2000)
5ht4r_human 4.57x57 153 TM4 S => A N/A N/A Mialet J et al (2000)
5ht4r_human 5.42x43 196 TM5 C => A N/A N/A Mialet J et al (2000)
5ht4r_human 5.43x44 197 TM5 S => A N/A N/A Mialet J et al (2000)
5ht4r_human 6.51x51 275 TM6 F => A N/A N/A Mialet J et al (2000)
5ht4r_human 6.52x52 276 TM6 F => V N/A N/A Mialet J et al (2000)
5ht4r_human 6.55x55 279 TM6 N => L N/A N/A Mialet J et al (2000)
5ht4r_human 7.43x42 302 TM7 Y => A N/A N/A Mialet J et al (2000)
5ht4r_human 6.55x55 279 TM6 N => L N/A N/A Mialet J et al (2000)
5ht4r_human 6.55x55 279 TM6 N => L N/A N/A Mialet J et al (2000)
5ht4r_human 6.55x55 279 TM6 N => L N/A N/A Mialet J et al (2000)
5ht4r_human 6.52x52 276 TM6 F => V N/A N/A Mialet J et al (2000)
5ht4r_human 6.52x52 276 TM6 F => V N/A N/A Mialet J et al (2000)
5ht4r_human 6.52x52 276 TM6 F => V N/A N/A Mialet J et al (2000)
5ht4r_human 6.52x52 276 TM6 F => V N/A N/A Mialet J et al (2000)
5ht4r_human 5.42x43 196 TM5 C => A N/A N/A Mialet J et al (2000)
5ht4r_human 5.42x43 196 TM5 C => A N/A N/A Mialet J et al (2000)
5ht4r_human 5.42x43 196 TM5 C => A N/A N/A Mialet J et al (2000)
5ht4r_human 5.42x43 196 TM5 C => A N/A N/A Mialet J et al (2000)
5ht4r_human 5.42x43 196 TM5 C => A N/A N/A Mialet J et al (2000)
5ht4r_human 4.57x57 153 TM4 S => A N/A N/A Mialet J et al (2000)
5ht4r_human 4.57x57 153 TM4 S => A N/A N/A Mialet J et al (2000)
5ht4r_human 4.57x57 153 TM4 S => A N/A N/A Mialet J et al (2000)
5ht4r_human 4.57x57 153 TM4 S => A N/A N/A Mialet J et al (2000)
5ht4r_human 4.54x54 150 TM4 T => V N/A N/A Mialet J et al (2000)
5ht4r_human 4.54x54 150 TM4 T => V N/A N/A Mialet J et al (2000)
5ht4r_human 4.54x54 150 TM4 T => V N/A N/A Mialet J et al (2000)
5ht4r_human 4.54x54 150 TM4 T => V N/A N/A Mialet J et al (2000)
5ht4r_human 3.32x32 100 TM3 D => N N/A N/A Mialet J et al (2000)
5ht4r_human 3.32x32 100 TM3 D => N N/A N/A Mialet J et al (2000)
5ht4r_human 3.32x32 100 TM3 D => N N/A N/A Mialet J et al (2000)
5ht4r_human 3.32x32 100 TM3 D => N N/A N/A Mialet J et al (2000)
5ht4r_human 2.50x50 66 TM2 D => N N/A N/A Mialet J et al (2000)
5ht4r_human 2.50x50 66 TM2 D => N N/A N/A Mialet J et al (2000)
5ht4r_human 2.50x50 66 TM2 D => N N/A N/A Mialet J et al (2000)
5ht4r_human 2.50x50 66 TM2 D => N N/A N/A Mialet J et al (2000)
5ht4r_human 2.50x50 66 TM2 D => N 26.316↓ K(i) (Binding - Radioligand competition/displacement) ML 10375 Mialet J et al (2000) Vass M et al (2019)
5ht4r_human 3.28x28 96 TM3 R => L 1.49↓ K(i) (Binding - Radioligand competition/displacement) ML 10375 Rivail L et al (2004) Vass M et al (2019)
5ht4r_human 3.32x32 100 TM3 D => N 62.5↓ K(i) (Binding - Radioligand competition/displacement) ML 10375 Mialet J et al (2000) Vass M et al (2019)
5ht4r_human 4.54x54 150 TM4 T => V 2.5↓ K(i) (Binding - Radioligand competition/displacement) ML 10375 Mialet J et al (2000) Vass M et al (2019)
5ht4r_human 4.57x57 153 TM4 S => A 1.499↓ K(i) (Binding - Radioligand competition/displacement) ML 10375 Mialet J et al (2000) Vass M et al (2019)
5ht4r_human 5.42x43 196 TM5 C => A 2.857↓ K(i) (Binding - Radioligand competition/displacement) ML 10375 Mialet J et al (2000) Vass M et al (2019)
5ht4r_human 6.52x52 276 TM6 F => V 2.857↓ K(i) (Binding - Radioligand competition/displacement) ML 10375 Mialet J et al (2000) Vass M et al (2019)
5ht4r_human 7.40x39 299 TM7 W => F 1.122↓ K(i) (Binding - Radioligand competition/displacement) ML 10375 Rivail L et al (2004) Vass M et al (2019)
5ht4r_human 2.50x50 66 TM2 D => N 6.757↓ K(i) (Binding - Radioligand competition/displacement) ML 10302 Mialet J et al (2000) Vass M et al (2019)
5ht4r_human 3.32x32 100 TM3 D => N 3.484↓ K(i) (Binding - Radioligand competition/displacement) ML 10302 Mialet J et al (2000) Vass M et al (2019)
5ht4r_human 4.54x54 150 TM4 T => V 1.393↑ K(i) (Binding - Radioligand competition/displacement) ML 10302 Mialet J et al (2000) Vass M et al (2019)
5ht4r_human 4.57x57 153 TM4 S => A 2.742↑ K(i) (Binding - Radioligand competition/displacement) ML 10302 Mialet J et al (2000) Vass M et al (2019)
5ht4r_human 5.42x43 196 TM5 C => A 4.722↑ K(i) (Binding - Radioligand competition/displacement) ML 10302 Mialet J et al (2000) Vass M et al (2019)
5ht4r_human 6.52x52 276 TM6 F => V 1.25↑ K(i) (Binding - Radioligand competition/displacement) ML 10302 Mialet J et al (2000) Vass M et al (2019)
5ht4r_human 6.55x55 279 TM6 N => L 2.297↑ K(i) (Binding - Radioligand competition/displacement) ML 10302 Mialet J et al (2000) Vass M et al (2019)
5ht4r_human 2.50x50 66 TM2 D => N 1.825↓ K(d) (Binding - Radioligand saturation) GR 113808 Mialet J et al (2000) Vass M et al (2019)
5ht4r_human 3.28x28 96 TM3 R => L 2.392↓ K(d) (Binding - Radioligand saturation) GR 113808 Rivail L et al (2004) Vass M et al (2019)
5ht4r_human 3.32x32 100 TM3 D => N 1.391↓ K(d) (Binding - Radioligand saturation) GR 113808 Mialet J et al (2000) Vass M et al (2019)
5ht4r_human 4.54x54 150 TM4 T => V 2.174↓ K(d) (Binding - Radioligand saturation) GR 113808 Mialet J et al (2000) Vass M et al (2019)
5ht4r_human 4.57x57 153 TM4 S => A 1.479↓ K(d) (Binding - Radioligand saturation) GR 113808 Mialet J et al (2000) Vass M et al (2019)
5ht4r_human 5.42x43 196 TM5 C => A 3.286↑ K(d) (Binding - Radioligand saturation) GR 113808 Mialet J et al (2000) Vass M et al (2019)
5ht4r_human 6.52x52 276 TM6 F => V 1.957↓ K(d) (Binding - Radioligand saturation) GR 113808 Mialet J et al (2000) Vass M et al (2019)
5ht4r_human 6.55x55 279 TM6 N => L 5.208↓ K(d) (Binding - Radioligand saturation) GR 113808 Mialet J et al (2000) Vass M et al (2019)
5ht4r_human 7.40x39 299 TM7 W => F 2.0↓ K(d) (Binding - Radioligand saturation) GR 113808 Rivail L et al (2004) Vass M et al (2019)
5ht4r_human 7.43x42 302 TM7 Y => F 13.333↓ K(d) (Binding - Radioligand saturation) GR 113808 Rivail L et al (2004) Vass M et al (2019)
5ht4r_human 3.28x28 96 TM3 R => L 2.392↓ K(i) (Binding - Radioligand competition/displacement) GR 113808 Rivail L et al (2004) Vass M et al (2019)
5ht4r_human 7.40x39 299 TM7 W => A N/A K(i) (Binding - Radioligand competition/displacement) GR 113808 Rivail L et al (2004) Vass M et al (2019)
5ht4r_human 7.40x39 299 TM7 W => F 2.0↓ K(i) (Binding - Radioligand competition/displacement) GR 113808 Rivail L et al (2004) Vass M et al (2019)
5ht4r_human 7.43x42 302 TM7 Y => F 13.333↓ K(i) (Binding - Radioligand competition/displacement) GR 113808 Rivail L et al (2004) Vass M et al (2019)
5ht4r_human 2.50x50 66 TM2 D => N 1.149↑ K(i) (Binding - Radioligand competition/displacement) 5-hydroxytryptamine Mialet J et al (2000) Vass M et al (2019)
5ht4r_human 3.32x32 100 TM3 D => N >125.0↓ K(i) (Binding - Radioligand competition/displacement) 5-hydroxytryptamine Mialet J et al (2000) Vass M et al (2019)
5ht4r_human 4.54x54 150 TM4 T => V 3.285↑ K(i) (Binding - Radioligand competition/displacement) 5-hydroxytryptamine Mialet J et al (2000) Vass M et al (2019)
5ht4r_human 4.57x57 153 TM4 S => A 1.351↓ K(i) (Binding - Radioligand competition/displacement) 5-hydroxytryptamine Mialet J et al (2000) Vass M et al (2019)
5ht4r_human 5.42x43 196 TM5 C => A 2.042↑ K(i) (Binding - Radioligand competition/displacement) 5-hydroxytryptamine Mialet J et al (2000) Vass M et al (2019)
5ht4r_human 6.52x52 276 TM6 F => V 1.111↑ K(i) (Binding - Radioligand competition/displacement) 5-hydroxytryptamine Mialet J et al (2000) Vass M et al (2019)
5ht4r_human 6.55x55 279 TM6 N => L >125.0↓ K(i) (Binding - Radioligand competition/displacement) 5-hydroxytryptamine Mialet J et al (2000) Vass M et al (2019)
5ht4r_human 3.28x28 96 TM3 R => L 1.624↑ K(i) (Binding - Radioligand competition/displacement) 5-hydroxytryptamine Rivail L et al (2004) Vass M et al (2019)
5ht4r_human 7.40x39 299 TM7 W => F 1.041↑ K(i) (Binding - Radioligand competition/displacement) 5-hydroxytryptamine Rivail L et al (2004) Vass M et al (2019)
5ht4r_human 3.28x28 96 TM3 R => L 25.641↓ K(i) (Binding - Radioligand competition/displacement) CHEMBL66114 Rivail L et al (2004) Vass M et al (2019)
5ht4r_human 7.40x39 299 TM7 W => F 1.522↓ K(i) (Binding - Radioligand competition/displacement) CHEMBL66114 Rivail L et al (2004) Vass M et al (2019)
5ht4r_human 7.43x42 302 TM7 Y => F 6.993↓ K(i) (Binding - Radioligand competition/displacement) CHEMBL66114 Rivail L et al (2004) Vass M et al (2019)
5ht4r_human 3.28x28 96 TM3 R => L 1.821↓ K(i) (Binding - Radioligand competition/displacement) RS 100235 Rivail L et al (2004) Vass M et al (2019)
5ht4r_human 7.40x39 299 TM7 W => F 1.005↓ K(i) (Binding - Radioligand competition/displacement) RS 100235 Rivail L et al (2004) Vass M et al (2019)
5ht4r_human 7.43x42 302 TM7 Y => F 1.918↑ K(i) (Binding - Radioligand competition/displacement) RS 100235 Rivail L et al (2004) Vass M et al (2019)
5ht4r_human 3.28x28 96 TM3 R => L 46.121↑ K(i) (Binding - Radioligand competition/displacement) ML11411 Rivail L et al (2004) Vass M et al (2019)
5ht4r_human 7.40x39 299 TM7 W => F 1.578↑ K(i) (Binding - Radioligand competition/displacement) ML11411 Rivail L et al (2004) Vass M et al (2019)
5ht4r_human 7.43x42 302 TM7 Y => F 1.49↓ K(i) (Binding - Radioligand competition/displacement) ML11411 Rivail L et al (2004) Vass M et al (2019)
5ht4r_human 3.28x28 96 TM3 R => A 2.571↓ pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
5ht4r_human 3.28x28 96 TM3 R => W 2.088↓ pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
5ht4r_human 3.32x32 100 TM3 D => A Abolished pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
5ht4r_human 3.36x36 104 TM3 T => A 166.667↓ pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
5ht4r_human 3.36x36 104 TM3 T => C 2.63↑ pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
5ht4r_human 3.37x37 105 TM3 T => A Abolished pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
5ht4r_human 45.52x52 186 ECL2 F => A 500.0↓ pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
5ht4r_human 5.39x40 193 TM5 A => F 26.316↓ pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
5ht4r_human 5.39x40 193 TM5 A => V 25.641↓ pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
5ht4r_human 5.42x43 196 TM5 C => A 1.905↓ pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
5ht4r_human 5.43x44 197 TM5 S => A 90.909↓ pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
5ht4r_human 6.48x48 272 TM6 W => A Abolished pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
5ht4r_human 6.51x51 275 TM6 F => A N/A pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
5ht4r_human 6.52x52 276 TM6 F => A 2.188↓ pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
5ht4r_human 6.52x52 276 TM6 F => V Abolished pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
5ht4r_human 6.55x55 279 TM6 N => A 1000.0↓ pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
5ht4r_human 6.55x55 279 TM6 N => S 500.0↓ pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
5ht4r_human 7.43x42 302 TM7 Y => A Abolished pEC50 (Functional - β-arrestin recruitment) 5-hydroxytryptamine Huang S et al (2022)
Protein name Generic number Segment Position Mutation FoldChange or Qual Exp Type Ligand Reference Review


Residue

Diagrams

ICL1 R Q L R K ICL1ECL1 I W I Y ECL1ICL2 P Q L V Y R N K M ICL2ECL2 W N N I G I I D L I E K R K F N Q N S N S T Y C V F M V ECL2ICL3 A S S E S R P Q S A D Q H S ICL3ECL3 D Y T V ECL3N-term M D K L D A N V S S E E G F G S N-termC-term D D E R Y R R P S I L G Q T V P C S T T T I N G S T H V L R D A V E C G G Q W E S Q C H P P A T S P L V A A Q P S D T C-term V E K V V L L T F L S T V I L M A I L G N L L V M V A V C W D I K T N Y F I V S L A F A D L L V S V L V M P F G A I E L V Q D G E V F C L V R T S L D V L L T T A S I F H L C C I S L D R Y Y A I C C T P L R I A L M L G G C W V I P T F I S F L P I M Q G N K P Y A I T C S V V A F Y I P F L L M V L A Y Y R I Y V T A K E H A H Q I Q M L Q R A G T H R M R T E T K A A K T L C I I M G C F C L C W A P F F V T N I V D P F I P G Q V W T A F L W L G Y I N S G L N P F L Y A F L N K S F L I F R R A I L C C
Download: PNG | SVG Increased binding/potency: >5-fold, >10-fold; Reduced binding/potency: >5-fold, >10-fold; No/low effect (<5-fold); and N/A
L N G L I A M L I V T S L F T L L V V K 1 V S L A F A D L L V S L V V M P F G A I E 2 C C L H F I S A T T L L V D L S T R V L 3 I A L M L G G C W V I P T F I S F L P I 4 Y A L V M L L F P I Y F A V V S C T I A Y 5 C I I M G C F C L C W A P F F V T N I V 6 F P N L G S N I Y G L W L F A T W V Q 7
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Residue Table


GPCRdb(A)
GPCRdb(A)
5-HT4 receptor
TM2
2x50 2.50x50 D66
TM3
3x28 3.28x28 R96
3x32 3.32x32 D100
3x36 3.36x36 T104
3x37 3.37x37 T105
TM4
4x53 4.53x53 P149
4x54 4.54x54 T150
4x57 4.57x57 S153
TM5
5x40 5.39x40 A193
5x43 5.42x43 C196
5x44 5.43x44 S197
TM6
6x48 6.48x48 W272
6x51 6.51x51 F275
6x52 6.52x52 F276
6x55 6.55x55 N279
TM7
7x39 7.40x39 W299
7x42 7.43x42 Y302